Assay Detail
Binding
CHEMBL661597
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In vitro inhibition of purified human C1r protease.
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Benzenesulfonamide derivatives of 2-substituted 4H-3,1-benzoxazin-4-ones and benzthiazin-4-ones as inhibitors of complement C1r protease.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 5.17 | 6.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL166801 | — | — | 1 | 6.16 |
| CHEMBL167523 | — | — | 1 | 5.82 |
| CHEMBL169044 | — | — | 1 | 5.55 |
| CHEMBL168038 | — | — | 1 | 5.50 |
| CHEMBL166632 | — | — | 1 | 5.40 |
| CHEMBL167163 | — | — | 1 | 5.22 |
| CHEMBL355466 | — | — | 1 | 5.16 |
| CHEMBL168702 | — | — | 1 | 5.12 |
| CHEMBL354950 | — | — | 1 | 5.11 |
| CHEMBL273264 | NAFAMOSTAT | 3.0 | 1 | 4.92 |
| CHEMBL354119 | — | — | 1 | 4.70 |
| CHEMBL165871 | — | — | 1 | 4.62 |
| CHEMBL165932 | — | — | 1 | 4.52 |
| CHEMBL165875 | — | — | 1 | 4.51 |
| CHEMBL354991 | — | — | 1 | - |
| CHEMBL353889 | — | — | 1 | - |
| CHEMBL167467 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL166801 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL167523 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL169044 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL168038 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL166632 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL167163 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL355466 | — | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL168702 | — | IC50 | = | 7500.0 | nM | 5.12 |
| CHEMBL354950 | — | IC50 | = | 7800.0 | nM | 5.11 |
| CHEMBL273264 | NAFAMOSTAT | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL354119 | — | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL165871 | — | IC50 | = | 24000.0 | nM | 4.62 |
| CHEMBL165932 | — | IC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL165875 | — | IC50 | = | 31000.0 | nM | 4.51 |
| CHEMBL354991 | — | IC50 | > | 62500.0 | nM | - |
| CHEMBL353889 | — | IC50 | > | 60000.0 | nM | - |
| CHEMBL167467 | — | IC50 | > | 62500.0 | nM | - |